Tpl2 kinase inhibitor [Ligand Id: 6051] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL200381
  • mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
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  • mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
ChEMBL Inhibitory activity against MEK B 4.4 pIC50 >40000 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5288-5292 [PMID:16165349]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR kinase autophosphorylation in A431 cells B 5.3 pIC50 <5000 nM IC50 Bioorg. Med. Chem. (2007) 15: 6425-6442 [PMID:17664070]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 6.6 pIC50 250 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4108-4114 [PMID:21632247]
mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279]
GtoPdb - - 7.3 pIC50 50 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5288-92 [PMID:16165349]
ChEMBL Inhibitory activity against human Tpl2 kinase via quantification of MEK phosphorylation F 7.3 pIC50 50 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5288-5292 [PMID:16165349]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]